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Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering.
Gu C, Lamb ML, Johannes JW, Sylvester MA, Eisman MS, Harrison RA, Hu H, Kazmirski S, Mikule K, Peng B, Su N, Wang W, Ye Q, Zheng X, Lyne PD, Scott DA. Gu C, et al. Among authors: lyne pd. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4775-4780. doi: 10.1016/j.bmcl.2016.08.030. Epub 2016 Aug 12. Bioorg Med Chem Lett. 2016. PMID: 27578247
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T, Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B, Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q, Yu Y, Zheng X, Scott DA. Johannes JW, et al. Among authors: lyne pd. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct 27. Bioorg Med Chem Lett. 2015. PMID: 26546219
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
Scott DA, Aquila BM, Bebernitz GA, Cook DJ, Dakin LA, Deegan TL, Hattersley MM, Ioannidis S, Lyne PD, Omer CA, Ye M, Zheng X. Scott DA, et al. Among authors: lyne pd. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4794-7. doi: 10.1016/j.bmcl.2008.07.093. Epub 2008 Jul 27. Bioorg Med Chem Lett. 2008. PMID: 18694641
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Dakin LA, Block MH, Chen H, Code E, Dowling JE, Feng X, Ferguson AD, Green I, Hird AW, Howard T, Keeton EK, Lamb ML, Lyne PD, Pollard H, Read J, Wu AJ, Zhang T, Zheng X. Dakin LA, et al. Among authors: lyne pd. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. doi: 10.1016/j.bmcl.2012.05.098. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22727640
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Gingipalli L, Block MH, Bao L, Cooke E, Dakin LA, Denz CR, Ferguson AD, Johannes JW, Larsen NA, Lyne PD, Pontz TW, Wang T, Wu X, Wu A, Zhang HJ, Zheng X, Dowling JE, Lamb ML. Gingipalli L, et al. Among authors: lyne pd. Bioorg Med Chem Lett. 2018 May 1;28(8):1336-1341. doi: 10.1016/j.bmcl.2018.03.018. Epub 2018 Mar 7. Bioorg Med Chem Lett. 2018. PMID: 29559278
Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer.
Wang Z, Grosskurth SE, Cheung T, Petteruti P, Zhang J, Wang X, Wang W, Gharahdaghi F, Wu J, Su N, Howard RT, Mayo M, Widzowski D, Scott DA, Johannes JW, Lamb ML, Lawson D, Dry JR, Lyne PD, Tate EW, Zinda M, Mikule K, Fawell SE, Reimer C, Chen H. Wang Z, et al. Among authors: lyne pd. Cancer Res. 2018 Dec 1;78(23):6691-6702. doi: 10.1158/0008-5472.CAN-18-1362. Epub 2018 Oct 8. Cancer Res. 2018. PMID: 30297535 Free article.
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M. Vasbinder MM, et al. J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23398453
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
Wang T, Lamb ML, Scott DA, Wang H, Block MH, Lyne PD, Lee JW, Davies AM, Zhang HJ, Zhu Y, Gu F, Han Y, Wang B, Mohr PJ, Kaus RJ, Josey JA, Hoffmann E, Thress K, Macintyre T, Wang H, Omer CA, Yu D. Wang T, et al. Among authors: lyne pd. J Med Chem. 2008 Aug 14;51(15):4672-84. doi: 10.1021/jm800343j. Epub 2008 Jul 23. J Med Chem. 2008. PMID: 18646745
41 results